IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC 50 of 0.5 nM.
性状
Solid
IC50 & Target[1][2]
EC50 Value: 0.5 nM
体外研究(In Vitro)
IWP-L6 (Porcn Inhibitor III) effectively suppressed the phosphorylation of dishevelled 2 (Dvl2) in HEK293 cells, a biochemical event associated with many Wnt-dependent cellular responses. IWP-L6 inhibits Wnt mediated branching morphogenesis in cultured embryonic kidneys . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
IWP-L6 (Porcn Inhibitor III) is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wang, X., et al., The development of highly potent inhibitors for porcupine. J Med Chem, 2013. 56(6): p. 2700-4.
溶解度数据
In Vitro: DMSO : 1.43 mg/mL (3.03 mM; Need ultrasonic)配制储备液